Hillsley K, Eeckhout C, Grundy D
Department of Biomedical Science, University of Sheffield, UK.
Neurosci Lett. 2000 Jan 14;278(3):137-40. doi: 10.1016/s0304-3940(99)00923-4.
The present study compares the efficacy of cilansetron, a 5-hydroxytryptamine (5-HT3)-receptor antagonist, delivered via intravenous and intraluminal routes, on the sensitivity of mesenteric afferent fibres supplying the proximal jejunum. Waveform analysis was performed to extract 5-HT sensitive single units from electrophysiological recordings of whole afferent nerve discharge. Dose effects of intravenous cilansetron (0.2-20 microg/kg) on the afferent response to 5-HT (10 microg) were examined to determine the threshold dose of cilansetron (2 microg/kg). This dose applied intraluminally to the region of jejunum innervated by the afferents, resulted in a greater degree of antagonism of the 5-HT response than intravenous administration (47.8+/-7.9 vs. 76.9+/-4.7%, P = 0.008). We concluded that cilansetron is active at its site of absorption to antagonize 5-HT3 receptors on vagal mucosal afferent terminals.
本研究比较了通过静脉内和腔内途径给药的5-羟色胺（5-HT3）受体拮抗剂西兰司琼对供应空肠近端的肠系膜传入纤维敏感性的影响。进行波形分析，从全传入神经放电的电生理记录中提取5-HT敏感的单个单位。研究静脉注射西兰司琼（0.2 - 20微克/千克）对5-HT（10微克）传入反应的剂量效应，以确定西兰司琼的阈值剂量（2微克/千克）。将该剂量腔内应用于由传入神经支配的空肠区域，与静脉给药相比，对5-HT反应的拮抗程度更大（47.8±7.9%对76.9±4.7%，P = 0.008）。我们得出结论，西兰司琼在其吸收部位具有活性，可拮抗迷走神经黏膜传入终末上的5-HT3受体。
